Drug intelligence / Profile preview

mesterolone

Development stage
Unknown
Lead developer
Bayer HealthCare Pharmaceuticals
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Mesterolone is a synthetic anabolic-androgenic steroid (AAS) and a derivative of dihydrotestosterone (DHT). It is primarily used in the treatment of male hypogonadism (low testosterone), androgen deficiency, oligozoospermia (low sperm count), Leydig cell failure, and infertility due to low natural hormone levels. Mesterolone acts as an agonist at the androgen receptor but is considered a weak androgen because it is rapidly inactivated by 3α-hydroxysteroid dehydrogenase in skeletal muscle. Unlike testosterone and some other AAS, mesterolone cannot be converted to estrogen via aromatase and therefore does not exhibit estrogenic effects. It was developed in the 1960s by Schering and introduced under the brand name Proviron. Mesterolone has also been studied for potential use in depression but remains mainly indicated for male hormone replacement therapy[1][2][4][5].

Brand names
ProvironPro-Viron
Other names
1α-methyl-4,5α-dihydrotestosterone1α-methyl-DHT1α-methyl-5α-androstan-17β-ol-3-onemestérolone
02

Targets

SHBG (Sex hormone-binding globulin)AR (Adrenergic receptors)

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